Eutectic-based self-nanoemulsified drug delivery system

• US 7,588,786 B2
• Filed: 11/14/2002
• Issued: 09/15/2009
• Est. Priority Date: 11/14/2001
• Status: Expired due to Fees

• Current Assignee: Jarrow Formulas Incorporated
• Original Assignee: Jarrow Formulas Incorporated
• Inventors: Nazzal, Sami, Khan, Mansoor A.
• Primary Examiner(s): Tate; Christopher R
• Assistant Examiner(s): WINSTON, RANDALL O
• Application Number:
  US10/293,932
• Publication Number:
  US 20030147927A1
• Time in Patent Office: 2,497 Days
• Field of Search: 424/400, 424/736, 514/11, 514/458, 514/633
• US Class Current: 424/736
• CPC Class Codes: A61K 31/12 Ketones
• CPC Class Codes: A61K 31/355 Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61P 3/02 Nutrients, e.g. vitamins, minerals
• CPC Class Codes: A61P 39/06 Free radical scavengers or antioxidants

Abstract

A eutectic-based self-nanoemulsified drug delivery system (SNEDDS) is formulated from polyoxyl 35 castor oil (Cremophor), medium chain mono- and diglycerides (capmul), essential oils, and a pharmacologically effective drug or nutraceutical or dietary supplement. The preferred pharmacologically effective drug is a poorly water soluble drug, such as ubiquinone (CoQ₁₀). The SNEDDS can be further incorporated into a powder to produce a solid dosage form. The solid dosage form contains the SNEDDS, a copolymer of vinylpyrrolidone and vinyl acetate (Kollidon VA 64), maltodextrin, and microcrystalline cellulose (MCC).

Claims

1. An orally administered dietary supplement including a eutectic-based delivery system, comprising:

a) ubiquinone; and

b) a sufficient amount of a volatile essential oil to solubilize the ubiquinone, and wherein said volatile essential oil is present in a sufficient amount to reduce the melting point of ubiquinone to 37°

C. or below, and thereby solubilize the ubiquinone comprised in the orally administered dietary supplement at or below body temperature.

2. The orally administered dietary supplement of claim 1, wherein said volatile essential oil is selected from the group consisting of menthol, spearmint oil, peppermint oil, lemon oil, anise oil, and mixtures thereof.

3. The orally administered dietary supplement of claim 1, further comprising a surfactant.

8. The orally administered dietary supplement of claim 1, wherein the dietary supplement composition is contained in a capsule.

13. The orally administered dietary supplement of claim 1, wherein the amount of the volatile essential oil is sufficient to solubilize the ubiquinone after ingestion by a patient.

4. A delivery system for pharmacologically effective agents, comprising:

a) ubiquinone;

b) a surfactant;

c) a sufficient amount of a volatile essential oil to reduce the melting point of ubiquinone to 37°

C. or below, and thereby solubilize the ubiquinone comprised in the delivery system at or below body temperature.

5. The eutectic-based delivery system of claim 4, wherein said volatile essential oil is selected from the group consisting of menthol, spearmint oil, peppermint oil, lemon oil, anise oil, and mixtures thereof.

6. The eutectic-based delivery system of claim 5, wherein said essential oil is lemon oil.

7. The eutectic-based delivery system of claim 4, wherein said surfactant is polyoxyl 35 caster oil or a medium chain mono- and diglyceride.

9. The eutectic-based delivery system of claim 4, wherein the delivery system is contained in a capsule.

10. An orally administered dietary supplement including a eutectic-based delivery system, comprising

a) ubiquinone;

and

b) a sufficient amount of a volatile essential oil to solubilize the ubiquinone, and wherein said volatile essential oil is present in a sufficient amount to reduce the melting point of ubiquinone to 37°

C. or below, and thereby solubilize the ubiquinone comprised in the orally administered dietary supplement at or below body temperature; and

c) wherein the dietary supplement composition is contained within a capsule.

11. The orally administered dietary supplement of claim 10, wherein the capsule is a hard capsule.

12. The orally administered dietary supplement of claim 10, wherein the capsule is a soft capsule.